This invention relates to novel nitrosourea derivatives which possess a high level of inhibitory activity against leukemia and other tumors and are therefore useful in therapeutic treatments of transplanted leukemic and tumor diseases. This invention further relates to a process for the preparation of such novel nitrosourea derivatives.
There are a variety of compounds which have been proposed as being effective for inhibiting leukemia and other tumors, of which one class is nitrosourea derivatives. Among the nitrosourea derivatives, there may be mentioned streptozotocin [N-(N'-methyl-N'-nitroso-carbamoyl)-D-glucosamine] and its derivatives such as methyl glucosaminides as being typical examples (refer to U.S. Pat. No. 3,577,406 and No. 3,767,640, for example), but they are not yet satisfactory because of insufficient activity against leukemia and other tumors, and/or undesirable side effects. Another class of nitrosourea derivatives is glycosyl derivatives of nitrosoureas which I have recently prepared and confirmed to be novel compounds, among which the most interesting compound is 1-(2-chloroethyl)-3-(.beta.-D-glucopyranosyl)-1-nitrosourea (abbreviated as GANU) which has a broad spectrum of antitumor activity against a variety of experimental tumors with shows good promise in its efficacy in human cancer chemotherapy (refer to T. Suami et al, U.S. Pat. No. 4,086,415).